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PF06869206

CAS No.
2227425-05-8
Chemical Name:
PF06869206
Synonyms
CS-2762;PF06869206;PF-06869206;PF-06869206; PF 06869206; PF06869206;inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206;(S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile;1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)-
CBNumber:
CB04187431
Molecular Formula:
C15H14ClF3N4O2
Molecular Weight:
374.75
MDL Number:
MFCD31657405
MOL File:
2227425-05-8.mol
Last updated:2024-11-19 23:02:33

PF06869206 Properties

Boiling point 599.2±50.0 °C(Predicted)
Density 1.57±0.1 g/cm3(Predicted)
storage temp. 2-8°C
solubility DMF: 1 mg/mL; DMSO: 1mg/mL; Ethanol: 10mg/mL; Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/mL
form A crystalline solid
pka 11.78±0.40(Predicted)
color White to off-white

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338

PF06869206 price More Price(19)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 28158 PF-06869206 2227425-05-8 1mg $32 2024-03-01 Buy
Cayman Chemical 28158 PF-06869206 2227425-05-8 25mg $533 2024-03-01 Buy
Cayman Chemical 28158 PF-06869206 2227425-05-8 5mg $139 2024-03-01 Buy
Cayman Chemical 28158 PF-06869206 2227425-05-8 10mg $243 2024-03-01 Buy
ChemScene CS-0043242 PF-06869206 99.85% 2227425-05-8 25mg $260 2021-12-16 Buy
Product number Packaging Price Buy
28158 1mg $32 Buy
28158 25mg $533 Buy
28158 5mg $139 Buy
28158 10mg $243 Buy
CS-0043242 25mg $260 Buy

PF06869206 Chemical Properties,Uses,Production

In Vivo

PF-06869206 is evaluated in rodent PK studies to determine suitability for in vivo pharmacology exploration. Results show moderate clearance in both rat and mouse. Oral bioavailability at 5 mg/kg is good in rat and moderate in mouse. At higher oral doses of 50 mg/kg, supraproportional increases in exposure are observed in both species, suggestive of saturation of clearance. PF-06869206 has moderate terminal elimination half-life (t1/2=1.35 h, and 0.75 h for Wistar-Han rats (10 mg/kg, iv), and C57BL6 mice (1 mg/kg, iv)). Furthermore, permeability is good (14×10-6 cm/s), and rat liver microsome (RLM) clearance is low (<14 μL/min/mg; HLM=39 μL/min/mg).

Description

PF-06869206 is an orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a; IC50 = 380 nM). It is selective for NaPi2a over NaPi2b, NaPi2c, PiT-1, and PiT-2 (IC50s = >25 μM).

Biological Activity

PF-06869206 (PF06869206) is a potent, selective, orally bioavailable inhibitor of sodium-phosphate cotransporter 2a (NaPi2a/SLC34A1) with IC50 of 380 nM, no inhibition against NaPi2b (SLC34A2) and NaPi2c (SLC34A3).PF-06869206 displays excellent subtype selectivity against other sodium-phosphate cotransporters: NaPi2b, NaPi2c, PiT-1, and PiT-2 (SLC20A2).PF-06869206 showed comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms (IC50=0.4-0.54 uM) and was selective over rodent NaPi2c, inhibited phosphate uptake in human proximal tubule cells.PF-06869206 was well tolerated and elicited a dose-dependent increase in fractional phosphate excretion, lowered plasma phosphate levels in WT mice and in rats with chronic kidney disease (CKD), induced an unabated acute phosphaturic and hypophosphatemic effect in CKD rats.

in vitro

PF-06869206 shows a balance of attributes with 380 nM NaPi2a inhibition potency, excellent subtype selectivity, and acceptable aqueous solubility (46 μM). PF-06869206 is profiled for potency in the rodent NaPi2a and NaPi2c cell lines. PF-06869206 shows comparable submicromolar activity for the human, rat, and mouse NaPi2a isoforms with IC50s of 0.4±0.047 μM and 0.54±0.099 μM for rat NaPi2a and mouse NaPi2a, respectively.

PF06869206 Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 41)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+undefined-21-51877795 ivan@atkchemical.com China 32957 60
Career Henan Chemica Co
+86-0371-86658258 +8613203830695 laboratory@coreychem.com China 30239 58
NINGBOBENKANGJS PHARMTECHCO., LTD
+8615990591583 15990591583 CHINA 2029 58
Zhejiang J&C Biological Technology Co.,Limited
+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10473 58
InvivoChem
+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6391 58
TargetMol Chemicals Inc.
support@targetmol.com United States 38631 58
Aladdin Scientific
+1-+1(833)-552-7181 sales@aladdinsci.com United States 57505 58
Wuhan Jingkang en Biomedical Technology Co., Ltd
+8613720134139 orders@jknbiochem.com China 5221 58
Fujian boshi pharmaceutical technology co. LTD 0595-22008920; 18120708884 393612455@qq.com China 255 58
Shanghai Lollane Biological Technology Co.,Ltd. 021-52996696,15000506266 15000506266 China 4566 55

View Lastest Price from PF06869206 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
PF-06869206 pictures 2024-11-19 PF-06869206
2227425-05-8
US $33.00-127.00 / mg 99.79% 10g TargetMol Chemicals Inc.
PF06869206 pictures 2024-10-22 PF06869206
2227425-05-8
US $0.01 / KG 1KG 95%-99% 1kg; 5kg; 10kg Career Henan Chemica Co
  • PF-06869206 pictures
  • PF-06869206
    2227425-05-8
  • US $33.00-127.00 / mg
  • 99.79%
  • TargetMol Chemicals Inc.
  • PF06869206 pictures
  • PF06869206
    2227425-05-8
  • US $0.01 / KG
  • 95%-99%
  • Career Henan Chemica Co

PF06869206 Spectrum

PF06869206 PF-06869206 CS-2762 PF-06869206; PF 06869206; PF06869206 1H-Pyrrolo[3,2-b]pyridine-6-carbonitrile, 3-chloro-7-[(2S)-2-(hydroxymethyl)-4-morpholinyl]-2-methyl-5-(trifluoromethyl)- (S)-3-Chloro-7-(2-(hydroxymethyl)morpholino)-2-methyl-5-(trifluoromethyl)-1H-pyrrolo[3,2-b]pyridine-6-carbonitrile inhibit,PF-06869206,Na+ channels,Sodium Channel,Na channels,PF 06869206,Inhibitor,PF06869206 2227425-05-8